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一些新型噻唑基-恶二唑啉的合成、亲脂性及抗菌活性评价

Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines.

作者信息

Stoica Cristina Ioana, IonuȚ Ioana, Pîrnău Adrian, Pop Carmen, Rotar AncuȚa, Vlase Laurian, Oniga Smaranda, Oniga Ovidiu

机构信息

Therapeutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.

出版信息

Clujul Med. 2015;88(4):521-9. doi: 10.15386/cjmed-473. Epub 2015 Nov 15.

Abstract

BACKGROUND AND AIMS

Synthesis of new potential antimicrobial agents and evaluation of their lipophilicity.

METHODS

Ten new thiazolyl-oxadiazoline derivatives were synthesized and their structures were validated by 1H-NMR and mass spectrometry. The lipophilicity of the compounds was evaluated using the principal component analysis (PCA) method. The necessary data for applying this method were obtained by reverse-phase thin-layer chromatography (RP-TLC). The antimicrobial activities were tested in vitro against four bacterial strains and one fungal strain.

RESULTS

The lipophilicity varied with the structure but could not be correlated with the antimicrobial activity, since this was modest.

CONCLUSIONS

We have synthesized ten new heterocyclic compounds. After their physical and chemical characterization, we determined their lipophilicity and screened their antimicrobial activity.

摘要

背景与目的

新型潜在抗菌剂的合成及其亲脂性评估。

方法

合成了十种新型噻唑基-恶二唑啉衍生物,并通过¹H-NMR和质谱对其结构进行了验证。使用主成分分析(PCA)方法评估了化合物的亲脂性。应用该方法所需的数据通过反相薄层色谱(RP-TLC)获得。对四种细菌菌株和一种真菌菌株进行了体外抗菌活性测试。

结果

亲脂性随结构变化,但由于抗菌活性适中,故无法与之建立相关性。

结论

我们合成了十种新型杂环化合物。在对其进行物理和化学表征后,测定了它们的亲脂性并筛选了抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/9202f94a5163/cm-88-521f1.jpg

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